WO1999063971B1 - Micro-osmotic controlled drug delivery systems - Google Patents

Micro-osmotic controlled drug delivery systems

Info

Publication number
WO1999063971B1
WO1999063971B1 PCT/US1999/013223 US9913223W WO9963971B1 WO 1999063971 B1 WO1999063971 B1 WO 1999063971B1 US 9913223 W US9913223 W US 9913223W WO 9963971 B1 WO9963971 B1 WO 9963971B1
Authority
WO
WIPO (PCT)
Prior art keywords
micro
pharmaceutical composition
drug delivery
therapeutic agent
delivery systems
Prior art date
Application number
PCT/US1999/013223
Other languages
French (fr)
Other versions
WO1999063971A1 (en
Inventor
Siva Narayan Tallavakhala
Original Assignee
Em Ind Inc
Siva Narayan Tallavakhala
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Em Ind Inc, Siva Narayan Tallavakhala filed Critical Em Ind Inc
Priority to DE1003485T priority Critical patent/DE1003485T1/en
Priority to AU46799/99A priority patent/AU4679999A/en
Priority to EP99930217A priority patent/EP1003485A1/en
Priority to JP2000553040A priority patent/JP2002517431A/en
Priority to CA002301042A priority patent/CA2301042A1/en
Publication of WO1999063971A1 publication Critical patent/WO1999063971A1/en
Publication of WO1999063971B1 publication Critical patent/WO1999063971B1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds

Definitions

  • a pharmaceutical composition comprising loaded cores comprising micro-osmotic cores having a coating of a drug component thereon, wherein the micro-osmotic cores comprise at least one micro-osmotic agent, wherein the drug component comprises at least one therapeutic agent, and wherein at least a portion of at least one therapeutic agent is in a solid-state solution in a mixture comprising a polyglycolyzed glycerides component and a polyoxypropylene- polyoxyethylene block co-polymer component.
  • micro- osmotic core further comprises at least one swelling agent or at least one gelling agent.
  • a pharmaceutical composition according to claim 1 wherein the portion of the therapeutic agent in a solid state solution comprises between 30% to 100% of the therapeutic agent in the drug component.
  • a pharmaceutical composition according to claim 1 wherein the loaded cores are combined with a polymer matrix.
  • a pharmaceutical composition according to claim 1 wherein the diameter of the loaded cores ranges from 2 ⁇ to 3 mm.
  • a pharmaceutical composition according to claim 1, wherein the therapeutic agent is a dihydropyridine compound.
  • a method of delivering at least one therapeutic agent to a physiologic target site comprising the steps of providing a pharmaceutical composition according to claim 1; and introducing a pharmaceutically effective amount of the pharmaceutical composition to the physiologic target site.
  • a method of delivering at least one therapeutic agent to a physiologic target site comprising the steps of providing a pharmaceutical composition according to claim 2; and introducing a pharmaceutically effective amount of the pharmaceutical composition to the physiologic target site.
  • a method of delivering at least one therapeutic agent to a physiologic target site comprising the steps of providing a pharmaceutical composition according to claim 3 and introducing a pharmaceutically effective amount of the pharmaceutical composition to the physiologic target site.
  • a method of formulating a pharmaceutical composition comprising the steps of providing a micro-osmotic core, coating the micro-osmotic core with a drug component, wherein the drug component comprises at least one therapeutic agent, wherein at least a portion of at least one therapeutic agent is in a solid-state solution in a mixture comprising a polyglycolyzed glycerides component and a polyoxypropylene- polyoxyethylene block co-polymer component.

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Disclosed herein are compositions and methods related to pharmaceutical compositions that employ a micro-osmotic core for the controlled delivery of a therapeutic agent. The invention particularly relates to therapeutic agents which are present in some portion in a solid state solution in the composition.

Description

- 36 - AMENDED CLAIMS
[received by the International Bureau on 16 December 1999 (16.12.99); original claims 1-21 replaced by amended claims 1-17 (3 pages)]
1. A pharmaceutical composition comprising loaded cores comprising micro-osmotic cores having a coating of a drug component thereon, wherein the micro-osmotic cores comprise at least one micro-osmotic agent, wherein the drug component comprises at least one therapeutic agent, and wherein at least a portion of at least one therapeutic agent is in a solid-state solution in a mixture comprising a polyglycolyzed glycerides component and a polyoxypropylene- polyoxyethylene block co-polymer component.
2. A pharmaceutical composition according to claim 1, wherein at least one micro-osmotic agent is sorbitol, mannitol, xylitol, or sodium chloride.
3. A pharmaceutical composition according to claim 1, wherein the micro- osmotic core further comprises at least one swelling agent or at least one gelling agent.
4. A pharmaceutical composition according to claim 1 , wherein the portion of the therapeutic agent in a solid state solution comprises between 30% to 100% of the therapeutic agent in the drug component.
5. A pharmaceutical composition according to claim 1, wherein the loaded cores are coated with a polymeric coating.
6. A pharmaceutical composition according to claim 1 , wherein the loaded cores are combined with a polymer matrix.
7. A pharmaceutical composition according to claim 1, wherein the loaded cores are coated with polymeric coating and combined with a polymer matrix. - 37 -
8. A pharmaceutical composition according to claim 1 , wherein the diameter of the loaded cores ranges from 2 μ to 3 mm.
9. A pharmaceutical composition according to claim 1, wherein the therapeutic agent is a dihydropyridine compound.
10. A method of delivering at least one therapeutic agent to a physiologic target site comprising the steps of providing a pharmaceutical composition according to claim 1; and introducing a pharmaceutically effective amount of the pharmaceutical composition to the physiologic target site.
11. A method according to claim 10, wherein the physiologic target site is the gastrointestinal tract.
12. A method of delivering at least one therapeutic agent to a physiologic target site comprising the steps of providing a pharmaceutical composition according to claim 2; and introducing a pharmaceutically effective amount of the pharmaceutical composition to the physiologic target site.
13. A method according to claim 12, wherein the physiologic target site is the gastrointestinal tract.
14. A method of delivering at least one therapeutic agent to a physiologic target site comprising the steps of providing a pharmaceutical composition according to claim 3 and introducing a pharmaceutically effective amount of the pharmaceutical composition to the physiologic target site.
15. A method according to claim 14, wherein the physiologic target site is the gastrointestinal tract. 16. A method of formulating a pharmaceutical composition comprising the steps of providing a micro-osmotic core, coating the micro-osmotic core with a drug component, wherein the drug component comprises at least one therapeutic agent, wherein at least a portion of at least one therapeutic agent is in a solid-state solution in a mixture comprising a polyglycolyzed glycerides component and a polyoxypropylene- polyoxyethylene block co-polymer component.
17. A method according to claim 16, wherein the portion of at least one therapeutic agent comprises 30% to 100%.
PCT/US1999/013223 1998-06-11 1999-06-11 Micro-osmotic controlled drug delivery systems WO1999063971A1 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
DE1003485T DE1003485T1 (en) 1998-06-11 1999-06-11 MICROOSMOTIC CONTROLLED DRUG DELIVERY SYSTEMS
AU46799/99A AU4679999A (en) 1998-06-11 1999-06-11 Micro-osmotic controlled drug delivery systems
EP99930217A EP1003485A1 (en) 1998-06-11 1999-06-11 Micro-osmotic controlled drug delivery systems
JP2000553040A JP2002517431A (en) 1998-06-11 1999-06-11 Micro-osmotic pressure controlled drug delivery system
CA002301042A CA2301042A1 (en) 1998-06-11 1999-06-11 Micro-osmotic controlled drug delivery systems

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8885598P 1998-06-11 1998-06-11
US60/088,855 1998-06-11

Publications (2)

Publication Number Publication Date
WO1999063971A1 WO1999063971A1 (en) 1999-12-16
WO1999063971B1 true WO1999063971B1 (en) 2000-02-10

Family

ID=22213892

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/013223 WO1999063971A1 (en) 1998-06-11 1999-06-11 Micro-osmotic controlled drug delivery systems

Country Status (8)

Country Link
EP (1) EP1003485A1 (en)
JP (1) JP2002517431A (en)
CN (1) CN1272785A (en)
AU (1) AU4679999A (en)
CA (1) CA2301042A1 (en)
DE (1) DE1003485T1 (en)
WO (1) WO1999063971A1 (en)
ZA (1) ZA200000610B (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9029144B2 (en) 2008-06-18 2015-05-12 Innovative Bio Therapies, Inc. Methods for enhanced propagation of cells

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10026698A1 (en) 2000-05-30 2001-12-06 Basf Ag Self-emulsifying active ingredient formulation and use of this formulation
EP2347756B1 (en) * 2001-07-06 2019-05-08 Veloxis Pharmaceuticals A/S Controlled agglomeration
AR039744A1 (en) * 2002-06-26 2005-03-09 Alza Corp METHODS AND DOSAGE FORMS TO INCREASE THE SOLUBILITY OF PHARMACOS COMPOSITIONS FOR CONTROLLED ADMINISTRATION
GB0222612D0 (en) * 2002-09-30 2002-11-06 Univ Gent Controlled delivery system for bioactive substances
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
US8377952B2 (en) 2003-08-28 2013-02-19 Abbott Laboratories Solid pharmaceutical dosage formulation
JP2007511518A (en) * 2003-11-13 2007-05-10 アルザ・コーポレーシヨン Melt blend dispersion
WO2005123039A1 (en) 2004-06-12 2005-12-29 Collegium Pharmaceutical, Inc. Abuse-deterrent drug formulations
JP2006327943A (en) * 2005-05-23 2006-12-07 Towa Yakuhin Kk Taste-masked tablet suppressed with delay of elution over time
CA2702904A1 (en) 2007-10-19 2009-04-23 Otsuka Pharmaceutical Co., Ltd. Matrix-type pharmaceutical solid preparation
US10668060B2 (en) 2009-12-10 2020-06-02 Collegium Pharmaceutical, Inc. Tamper-resistant pharmaceutical compositions of opioids and other drugs
US20190060325A1 (en) * 2016-04-08 2019-02-28 Shionogi & Co., Ltd. Stabilized solid dosage form
WO2017222575A1 (en) 2016-06-23 2017-12-28 Collegium Pharmaceutical, Inc. Process of making more stable abuse-deterrent oral formulations

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4758437A (en) * 1981-12-23 1988-07-19 Yamanouchi Pharmaceutical Co., Ltd. Composition for long acting nicardipine preparation and process of producing the composition
US5260068A (en) * 1992-05-04 1993-11-09 Anda Sr Pharmaceuticals Inc. Multiparticulate pulsatile drug delivery system
IE80467B1 (en) * 1995-07-03 1998-07-29 Elan Corp Plc Controlled release formulations for poorly soluble drugs
HUP9903869A3 (en) * 1996-06-28 2000-07-28 Schering Corp Oral composition comprising a triazole antifungal compound

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9029144B2 (en) 2008-06-18 2015-05-12 Innovative Bio Therapies, Inc. Methods for enhanced propagation of cells

Also Published As

Publication number Publication date
ZA200000610B (en) 2001-06-11
AU4679999A (en) 1999-12-30
DE1003485T1 (en) 2000-11-02
CA2301042A1 (en) 1999-12-16
EP1003485A1 (en) 2000-05-31
CN1272785A (en) 2000-11-08
WO1999063971A1 (en) 1999-12-16
JP2002517431A (en) 2002-06-18

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